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    Pyridyl-substituted spiro-hydantoin crystalline forms and process
    1.
    发明申请
    Pyridyl-substituted spiro-hydantoin crystalline forms and process 审中-公开
    吡啶基取代的螺 - 乙内酰脲结晶形式及方法

    公开(公告)号：US20060142319A1

    公开(公告)日：2006-06-29

    申请号：US11301433

    申请日：2005-12-13

    申请人： Bang-Chi Chen ,  Albert Delmonte ,  T.G. Dhar ,  Michael Galella ,  Margaret Gleeson ,  Jack Gougoutas ,  Douglas McLeod ,  Huiping Zhang

    发明人： Bang-Chi Chen ,  Albert Delmonte ,  T.G. Dhar ,  Michael Galella ,  Margaret Gleeson ,  Jack Gougoutas ,  Douglas McLeod ,  Huiping Zhang

    IPC分类号： A61K31/4747 ,  C07D487/10

    CPC分类号： C07D487/10

    摘要： The invention provides crystalline forms of 6-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl]nicotinic acid, its pharmaceutically acceptable salts, or solvates, thereof Further, a process is provided for preparing substituted spiro-hydantoin compounds of the formula I wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A1, A2, G, and Q are linkers; and R2, R4a, R4c, and R16 are defined in the specification. The process includes the reaction of N-substituted glycine compound and methylene precursor compound with an alkene compound. The substituted spiro-hydantoin compounds of formulae I and II are useful in the treatment of immune and/or inflammatory diseases.

    摘要翻译： 本发明提供6 - [（5S，9R）-9-（4-氰基苯基）-3-（3,5-二氯苯基）-1-甲基-2,4-二氧代-1,3,7-三氮杂螺[ [4.4]非7-基]烟酸，其药学上可接受的盐或溶剂化物。此外，提供了制备式I的取代的螺 - 乙内酰脲化合物的方法，其中Z是N或CR 4b， SUB>; K和L独立地为O或S; Ar是任选取代的芳基或杂芳基; A 1，A 2，G和Q是连接体; 和R 2，R 4a，R 4c和R 16在本说明书中定义。 该方法包括N-取代的甘氨酸化合物和亚甲基前体化合物与烯烃化合物的反应。 式I和II的取代的螺 - 乙内酰脲化合物可用于治疗免疫和/或炎性疾病。